Back to results
US 12,662,475 B2Granted
Difluorocyclohexyl derivatives as IL-17 modulators
AssigneeUcb Biopharma Srl
InventorsPrafulkumar Tulshibhai Chovatia, Anne Marie Foley, Martin Clive Hutchings, James Andrew Johnson, Fabien Claude Lecomte, Nathaniel Julius Thomas Monck, James Thomas Reuberson, Adam Peter Smalley, Darshan Gunvant Vaidya
Life of this patent
Estimating the term…
Abstract
A series of substituted 4,4-difluorocyclohexyl derivatives as defined herein, being potent modulators of human IL-17 activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including inflammatory and autoimmune disorders.
Claims9
A compound of formula (IIA) or an N-oxide thereof, or a pharmaceutically acceptable salt thereof:
- wherein
- A represents C—R1 or N;
- E represents C—R2 or N;
- R1 represents hydrogen or fluoro;
- R2 represents hydrogen or fluoro;
- R3 represents —NR3aR3b;
- or R3 represents a group of formula (Wa):
- in which the asterisk (*) represents the point of attachment to the remainder of the molecule;
- W represents the residue of an optionally substituted saturated monocyclic ring containing 3 to 6 carbon atoms, one nitrogen atom, and 0, 1, 2 or 3 additional heteroatoms independently selected from N, O and S, but containing no more than one O or S atom;
- or
- W represents the residue of an optionally substituted saturated bicyclic ring system containing 4 to 10 carbon atoms, one nitrogen atom, and 0, 1, 2 or 3 additional heteroatoms independently selected from N, O and S, but containing no more than one O or S atom;
- or
- W represents the residue of an optionally substituted saturated spirocyclic ring system containing 5 to 10 carbon atoms, one nitrogen atom, and 0, 1, 2 or 3 additional heteroatoms independently selected from N, O and S, but containing no more than one O or S atom;
- R3a represents hydrogen or C1-6 alkyl;
- R3b represents C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl(C1-6)alkyl, aryl, aryl(C1-6)alkyl, C3-7 heterocycloalkyl, C3-7 heterocycloalkyl(C1-6)alkyl, heteroaryl or heteroaryl(C1-6)alkyl, any of which groups may be optionally substituted by one or more substituents;
- R4a represents hydrogen, fluoro or hydroxy;
- or R4a represents C1-6 alkyl, which group may be optionally substituted by one or more substituents;
- and
- R4b represents hydrogen, fluoro or C1-6 alkyl;
- or
- R4a and R4b, when taken together with the carbon atom to which they are both attached, represent C3-9 cycloalkyl or C3-7 heterocycloalkyl, either of which groups may be optionally substituted by one or more substituents;
- and
- R16 represents methyl, ethyl, isopropyl or cyclopropyl.
20 more elements
Dependencies are inferred from the claim text.